The ChEMBL-og

Wikipedia: Eslicarbazepine Acetate On November 8th 2013, FDA approved Eslicarbazepine Acetate (tradename: Aptiom ; research codes: Sep-0002093, BIA 2-093; ChEMBL: CHEMBL87992 ), a prodrug indicated as adjunctive treatment of partial-onset seizures associated with epilepsy . Epilepsy is neurological disorder characterised by abnormal neuronal activity in the brain. Partial-onset seizures, as opposed to generalised seizures , affect initially only one part of the brain and, depending on the part of the brain that is affected, these seizures will present different symptoms. Eslicarbazepine (ChEMBL: CHEMBL315985 ), the bioactive ingredient of the prodrug Eslicarbazepine Acetate, exerts its anticonvulsant activity by blocking the voltage-gated sodium channel (VGSC) . VGSC has 3 distinctive states: the resting state, during which the VGSC is closed but responsive to a depolarisation impulse, the open state, during which the channel is open allowing the sodium ion to enter the cel...

ATC code S01EE05 Wikipedia Tafluprost On Feb 13th, 2012 FDA approved Tafluprost ( trade name Zioptan) for treatment of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Tafluprost had been already available under the trade name Taflotan in Germany and Denmark from 2008, and under the trade name Saflutan in the United Kingdom and Spain from 2009. Glaucoma is an eye disease associated with increased fluid pressure in the eye, eventually causing permament damage to the optic nerve, impairing the field of vision and ultimately leading to blindness. Glaucomas can be sub-classified as open-angle glaucoma (OAG) and closed-angle glaucoma (CAG), with OAG being a slowly progressive disease responsible for ~90% of glaucoma cases in the US, and CAG being an acute disease with rapid progression. Alongside various surgical forms of treatment, management of OAG usually consists of medication to lower intraocular pressure. Taf...

ATC code (partial): G03   On 28th April 2011, the FDA approved Abiraterone acetate (Brand name Zytiga TM , NDA 202379) for the treatment of castrate-resistant prostate cancer (CRPC). Specifically, it is indicated for use in combination with prednisone for the treatment of patients with metastatic CRPC who have received prior chemotherapy containing docetaxel. Response biomarkers are amplified Androgen Receptor (AR); PTEN loss and hormone driven ERG rearrangement. Abiraterone acetate (research code: CB-7630) is a steroid derivative with a chemical formula C26H33NO, (IUPAC: (3β)­ 17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate; SMILES= (CC(=O)O[C@H]1CC[C@]2(C)[C@H]3CC[C@@]4(C)[C@@H](CC=C4c5cccnc5)[C@@H]3CC=C2C1 ); InChI=1S/C26H33NO2/c1-17(28)29-20-10-12-25(2)19(15-20)6-7-21-23-9-8-22(18-5-4-14-27-16-18)26(23,3)13-11-24(21)25/h4-6,8,14,16,20-21,23-24H,7,9-13,15H2,1-3H3/t20-,21-,23-,24-,25-,26+/m0/s1). It has molecular weight 391.55 and a LogP of 5.12. Abiraterone ...

ATC code (partial): N03AX    On April 6th, the FDA approved gabapentin enacarbil (tradename Horizant , Research Code: XP-13512, NDA 022399) for the treatment of moderate-severe forms of restless legs syndrome (RLS). Patients suffering from RLS experience an urge to move their legs or other limbs. This urge is prompted by a painful or itchy sensation in the corresponding limb. Symptoms are most severe during phases of relaxation. Patients also sometimes have limb jerking during sleep. Gabapentin enacarbil is a prodrug of the anticonvulsant and analgesic gabapentin ( CHEMBL940 ). Much of the processing of gabapentin enacarbil into the active ingredient takes place in enterocytes, upon absorption in the gut. These first pass modifications are mainly mediated by non-specific carboxylesterases and via several steps of hydrolysis and yield gabapentin (the active ingredient), along with carbon dioxide, acetaldehyde and isobutyric acid. Absorption of Gabapentin ...